This project describes the intramural formulation activities with potential antineoplastic agents. Primarily, these studies were directed toward evaluation of stability of certain new antitumor agents and resolution of particular solubility problems. Hydrolysis of two bischloroethyl containing alkylating agents (Spirohydantoin mustard and Melphalan) were studied. Spriohydantoin mustard rapidly hydrolyzed in aqueous solution. Chloride ion reduced the rate of hydrolysis but only the addition of a 10% o/w emulsion reduced decomposition to a degree sufficient to use clinically. Melphalan was significantly more stable even under conditions used for local hyperthermia (41 degrees C). Formulation studies leading to soluble stable formulations of diamorphine and morphine were carried out. Although certain excipients (sodium phosphate, mannitol) accelerated diamorphine decomposition, lactose provided a stable lyophilized dosage form. A suitable lyophilized dosage form of morphine acetate was also prepared. Reconstitution yielded solutions of high solubility (greater than 100 mg/ml) and acceptable stability. A water soluble prodrug derivative of NSC-282175, 4-hydroxy androst-4-ene-3,17-dione, was prepared. The succinic acid hemiester and sodium salt of the ester were 10 and 700 times as soluble. Under physiologic conditions, facile reversion to NSC-282175 was demonstrated.